- Highly Stereoselective Synthesis of trans -Dihydronarciclasine Analogues
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Several new trans -dihydronarciclasine analogues were stereo selectively synthesised by applying our feasible and efficient process developed recently. These new phenanthridone alkaloid derivatives were obtained in both racemic and optically active forms. During their enantioselective syntheses, high selectivities (up to 99% ee) were achieved by using (8 S,9 S)-9-amino(9-deoxy)epiquinine as an organocatalyst. The modifications, the introduction of ethoxy or methoxy groups, were made in ring A of the phenanthridone scaffold.
- Varró, Gábor,Mattyasovszky, Lenke,Grün, Alajos,Simon, András,Hegedüs, László,Kádas, István
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p. 625 - 643
(2017/11/27)
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- Solvent-free, visible-light photocatalytic alcohol oxidations applying an organic photocatalyst
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A method for the solvent-free photocatalytic conversion of solid and liquid substrates was developed, using a novel rod mill apparatus. In this setup, thin liquid films are realized which is crucial for an effective photocatalytic conversion due to the low penetration depth of light in heterogeneous systems. Several benzylic alcohols were oxidized with riboflavin tetraacetate as photocatalyst under blue light irradiation of the reaction mixture. The corresponding carbonyl compounds were obtained in moderate to good yields.
- Obst, Martin,K?nig, Burkhard
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p. 2358 - 2363
(2016/12/07)
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- Design and synthesis of EGFR dimerization inhibitors and evaluation of their potential in the treatment of psoriasis
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Hit compounds from in silico screening for inhibitors of the EGFR dimerization process were evaluated for their anti-proliferative (CCD-1106 keratinocytes) and anti-oxidant (TBA assay) activity and their effect on EGFR dimerization (BS3 chemical crosslinking assay). 7-Benzyl-8-{N′- [1-(3-ethoxy-4-hydroxyphenyl)meth-(Z)-ylidene]hydrazino}-1,3-dimethylxanthine 2a (127 μM) leads to 37% inhibition of p-EGFR dimerization in the CCD-1106 cell line and also inhibits phosphorylation of proteins in the MAPK/ERK pathway, ERK 1/2 and p-38. Based on this initial data, 2a was selected for further study and was evaluated for its anti-proliferative activity in a range of keratinocyte (CCD-1106, HaCaT and NHEK) and monocyte (ThP1 and U937) cell lines. Xanthine 2a is pro-apoptotic in HaCaT keratinocytes, as shown by electron microscopy, caspase 3/7, and annexin V-FITC/PI flow cytometric assays. It is significantly less cytotoxic than the established antipsoriatic agent dithranol 14, as determined by MTT and LDH release assays, and thus has potential as a lead compound for the treatment of psoriasis.
- Petch, Donna,Anderson, Rosaleen J.,Cunningham, Anne,George, Suja E.,Hibbs, David E.,Liu, Ran,MacKay, Simon P.,Paul, Andrew,Small, David A.P.,Groundwater, Paul W.
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p. 5901 - 5914
(2012/11/06)
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- Electroluminescent liquid crystals
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A new class of liquid crystals for use as transport layers and/or emission layers in organic light-emitting diodes has been prepared. Depending on the nature and number of the terminal substituents enatiotropic nematic, smectic and columnar phases are observed. Chain branching gives rise to materials with a low melting point. Several of these liquid crystals electroluminesce in the visible region. The charge transport properties of some of these materials have been evaluated.
- Contoret, Adam,Eastwood, Amanda,Farrar, Simon,Kelly, Stephen M.,Nicholls, Edward,O'Neill, Mary,Richards, Gary,Wu, Catherine
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p. 271 - 278
(2007/10/03)
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